Pyrrolylquinoxalinediones: A new class of AMPA receptor antagonists

✍ Scribed by W. Lubisch; B. Behl; H.P. Hofmann

• Book ID: 104364680
• Publisher: Elsevier Science
• Year: 1996
• Tongue: English
• Weight: 295 KB
• Volume: 6
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/s0960-894x(96)00534-3

✦ Synopsis

Pyrrolylquinoxalinediones were synthesized and their affinities for the AMPA receptor were determined. Most compounds showed moderate to good affinities. The acetic acid derivative 8b exhibited a K~ value of 70 nM and was equipotent to NBQX 1. Structure activity relationships are discussed. Selected compounds were tested for their potency to inhibit AMPA induced lethal convulsions in mice. In this in vivo model the compounds showed improved potency compared with NBQX.